TABLE 2.
IC50s determined by ATPase and triplex formation assays
| Compound | IC50 (nM) by:
|
Ratioc | Concn (μM) required for fourfold or greater induction in reporter gene assays
|
||
|---|---|---|---|---|---|
| ATPase assaya | Triplex formation assayb | gyrA promoter fusion | sulA promoter fusion | ||
| Novclobiocin 201 | 65 ± 7 | 17 ± 1 | 3.8 | 13 | 6.3 |
| Novclobiocin 601 | 72 ± 6 | <5 ± 0.7 | NDd | 3.1 | 3.1 |
| Clorobiocin | 73 ± 5 | <5 ± 0.2 | ND | 1.6 | <1 |
| Novclobiocin 241 | 73 ± 6 | 41 ± 11 | 1.8 | 3.1 | 3.1 |
| Novclobiocin 217 | 84 ± 5 | 19 ± 6 | 4.4 | 3.1 | 1.6 |
| Novclobiocin 371 | 84 ± 5 | 20 ± 10 | 4.2 | 3.1 | 12.5 |
| Novclobiocin 314 | 86 ± 8 | 25 ± 2 | 3.4 | 12.5 | 12.5 |
| Novclobiocin 701 | 90 ± 20 | 34 ± 6 | 2.7 | 6.3 | 3.1 |
| Novclobiocin 703 | 106 ± 24 | ND | ND | NIe | 50 |
| Novclobiocin 225 | 116 ± 6 | 34 ± 6 | 3.4 | 1.6 | 3.1 |
| Novclobiocin 311 | 122 ± 8 | 22 ± 6 | 5.6 | 25 | 6.3 |
| Novclobiocin 604 | 131 ± 4 | ND | ND | 6.3 | 6.3 |
| Novclobiocin 741 | 137 ± 15 | 32 ± 4 | 4.3 | 25 | 25 |
| Novclobiocin 386 | 152 ± 27 | 44 ± 8 | 3.5 | 25 | 50 |
| Novobiocin | 154 ± 10 | 200 ± 20 | 0.8 | 3.1 | 6.3 |
| Novclobiocin 313 | 185 ± 10 | 75 ± 10 | 2.5 | 25 | 25 |
| Novclobiocin 603 | 219 ± 10 | 50 ± 10 | 4.4 | 50 | 50 |
| Novclobiocin 203 | 229 ± 39 | 120 ± 20 | 1.9 | >100 | NI |
| Novclobiocin 731 | 263 ± 53 | 43 ± 4 | 6.1 | 6.3 | 3.1 |
| Novclobiocin 742 | 276 ± 36 | 280 ± 70 | 1.0 | 50 | 50 |
| Novclobiocin 372 | 280 ± 19 | ND | ND | NI | 12.5 |
| Novclobiocin 602 | 297 ± 42 | 110 ± 40 | 2.7 | >100 | 50 |
| Novclobiocin 202 | 376 ± 172 | 320 ± 70) | 1.2 | 100 | 100 |
| Novclobiocin 702 | 598 ± 144 | 1,200 ± 200 | 0.5 | >100 | NI |
| Novclobiocin 218 | 758 ± 67 | 140 ± 30 | 5.4 | 25 | 100 |
| Novclobiocin 387 | 784 ± 43 | 190 ± 40 | 4.1 | >100 | 100 |
| Novclobiocin 312 | 891 ± 82 | 460 ± 70 | 1.9 | NI | 100 |
| Novclobiocin 226 | 2,787 ± 512 | 460 ± 100 | 6.1 | NI | 100 |
| Novclobiocin 204 | >10,000 | ND | ND | NI | NI |
| Novclobiocin 219 | >10,000 | ND | ND | 3.1 | NI |
| Novclobiocin 315 | >10,000 | ND | ND | NI | NI |
| Novclobiocin 606 | >10,000 | ND | ND | NI | NI |
| Novclobiocin 704 | >10,000 | ND | ND | NI | NI |
a
The values represent the means ± standard deviations. Grafit 5 software was used to calculate IC50s from single data points obtained at eight different concentrations.
b
The values represent the means ± standard errors of the means. Sigma Plot (version 10) software was used to calculate IC50s from duplicate or triplicate data points obtained at eight different concentrations.
c
Ratio of the IC50 by the ATPase assay to the IC50 by the triplex formation assay.
d
ND, not determined.
e
NI, no induction was observed.